GW806742X is a potent MLKL inhibitor, also a human and murine necroptosis inhibitor. GW806742X binds the MLKL pseudokinase domain with a Kd value of 9.3 μM and has anti-necroptosis activity. GW806742X has activity against VEGFR2. GW806742X blocked necroptosis and IL-33 release in vitro and reduced eosinophilia in Aspergillus fumigatus extract-induced asthma in vivo, an allergic inflammation model that is highly dependent on IL-33.
CAS Number: 579515-63-2
Molecular Weight: 573.55
Chemical Name: GW806742X
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
GW806742X (0.1-10000 nM) rescues 50% of wild-type mouse dermal fibroblasts (MDFs) from TSQ-induced necroptosis with an IC50< 50 nM when 1 ng/mL TNF is used. GW806742X (1 μM) retards MLKL translocation to the membrane.
- Hildebrand JM, et al. Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death. Proc Natl Acad Sci U S A. 2014 Oct 21;111(42):15072-7.
- Yan B, et al. Discovery of a new class of highly potent necroptosis inhibitors targeting the mixed lineagekinase domain-like protein. Chem Commun (Camb). 2017 Mar 28;53(26):3637-3640.
Products are for research use only. Not for human use.
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